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    Cephalosporins
    4.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4992431A

    公开(公告)日：1991-02-12

    申请号：US393761

    申请日：1982-06-30

    Applicant: Rene Heymes ,  Didier Pronine

    Inventor： Rene Heymes ,  Didier Pronine

    IPC: C07D501/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D501/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36

    CPC classification number: C07D277/587 ,  C07D501/34 ,  C07D501/36 ,  Y02P20/55

    Abstract: Novel syn isomers of 3-alkoxymethyl or 3-alkylthiomethyl-7-[2-(2-amino-4-thiazolyl)-2-oximino-acetamido]-cephalosporanic acid compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and alkoxy carbonyl of 2 to 6 carbon atoms, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.4, magnesium, non-toxic, pharmaceutically acceptable organic amine and an easily cleavable ester group, Ra' is selected from the group consisting of alkyl of 1 to 6 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 6 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms, n is 0, 1 or 2, X' is selected from the group consisting of oxygen and sulfur optionally oxidized to sulfoxide or sulfone and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity and their preparation.

    Abstract translation: 其中R选择的3-烷氧基甲基或3-烷基硫甲基-7- [2-（2-氨基-4-噻唑基）-2-肟基 - 乙酰氨基] - 大环离子型环孢菌素的新颖的同异构体 由碳原子数1〜6的烷基，碳原子数2〜6的烯基和炔基，碳原子数3〜6的环烷基，碳原子数1〜18的有机羧酸的酰基和烷氧基羰基2 至少6个碳原子，A选自氢，碱金属，碱土金属，-NH 4，镁，无毒，药学上可接受的有机胺和易裂解的酯基，Ra'选自 1至6个碳原子的烷基，任选被杂原子，2至6个碳原子的烯基和炔基以及7至12个碳原子的任选取代的芳烷基间隔，n为0,1或2，X'选自 的氧和硫任选地被氧化成亚砜或砜及其无毒的制药 可接受的具有抗生素活性的酸加成盐及其制备方法。

    2-Amino-4-thiazolyl-2-oxyimino-acetamido-bicyclooctene-carboxylic acids
    5.
    发明授权
    2-Amino-4-thiazolyl-2-oxyimino-acetamido-bicyclooctene-carboxylic acids 失效
    2-氨基-4-噻唑基-2-氧亚氨基 - 乙酰氨基 - 双环辛烯 - 羧酸

    公开(公告)号：US4476124A

    公开(公告)日：1984-10-09

    申请号：US377597

    申请日：1982-05-12

    Applicant: Rene Heymes ,  Alain Bonnet ,  Didier Pronine

    Inventor： Rene Heymes ,  Alain Bonnet ,  Didier Pronine

    IPC: C07D507/04 ,  A61K31/535 ,  A61K31/54 ,  A61P31/04 ,  C07D498/04 ,  C07D501/20 ,  C07D507/06 ,  C07D507/08 ,  C07D513/04 ,  C07D417/12

    CPC classification number: C07D513/04

    Abstract: Novel syn isomers of optically active isomers and racemates of 7-[2-(2-amino-4-thiazolyl)-2-oxyimino-acetamido]-bicyclooctene-carboxylic acid derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, methyl, halomethyl, hydroxymethyl and acyloxymethyl, X is selected from the group consisting of oxygen and optionally oxidized sulfur, A is selected from the group consisting of hydrogen, an alkali metal, --NH.sub.4, alkaline earth metal equivalent, a non-toxic, pharmaceutically acceptable organic amine and an easily cleavable ester group and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity and their preparation.

    Abstract translation: 式（I）的7- [2-（2-氨基-4-噻唑基）-2-氧亚氨基 - 乙酰氨基] - 双环辛烯 - 羧酸衍生物的光学活性异构体和外消旋体的新型顺式异构体，其中R选自 由氢，任选取代的1至6个碳原子的烷基和任选取代的2至6个碳原子的烯基和炔基组成的基团，R 1选自氢，甲基，卤代甲基，羟甲基和酰氧基甲基，X选自 A由氧，碱金属，-NH4，碱土金属当量，无毒的药学上可接受的有机胺和易裂解的酯基组成的组中选择， 具有抗生素活性的有毒，药学上可接受的酸加成盐及其制备。

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